Mapping the Biotransformation of Coumarins through Filamentous Fungi

Natural coumarins are present in remarkable amounts as secondary metabolites in edible and medicinal plants, where they display interesting bioactivities. Considering the wide enzymatic arsenal of filamentous fungi, studies on the biotransformation of coumarins using these microorganisms have great importance in green chemical derivatization. Several reports on the biotransformation of coumarins using fungi have highlighted the achievement of chemical analogs with high selectivity by using mild and ecofriendly conditions. Prompted by the enormous pharmacological, alimentary, and chemical interest in coumarin-like compounds, this study evaluated the biotransformation of nine coumarin sca olds using Cunninghamella elegans ATCC 10028b and Aspergillus brasiliensis ATCC 16404. The chemical reactions which were catalyzed by the microorganisms were highly selective. Among the nine studied coumarins, only two of them were biotransformed. One of the coumarins, 7-hydroxy-2,3-dihydrocyclopenta[c]chromen-4(1H)-one, was biotransformed into the new 7,9-dihydroxy-2,3-dihydrocyclopenta[c]chromen-4(1H)-one, which was generated by selective hydroxylation in an unactivated carbon. Our results highlight some chemical features of coumarin cores that are important to biotransformation using filamentous fungi

In Silico Antiprotozoal Evaluation of 1,4-Naphthoquinone Derivatives against Chagas and Leishmaniasis Diseases Using QSAR, Molecular Docking, and ADME Approaches

Chagas and leishmaniasis are two neglected diseases considered as public health problems worldwide, for which there is no effective, low-cost, and low-toxicity treatment for the host. Naphthoquinones are ligands with redox properties involved in oxidative biological processes with a wide variety of activities, including antiparasitic. In this work, in silico methods of quantitative structure–activity relationship (QSAR), molecular docking, and calculation of ADME (absorption, distribution, metabolism, and excretion) properties were used to evaluate naphthoquinone derivatives with unknown antiprotozoal activity. QSAR models were developed for predicting antiparasitic activity against Trypanosoma cruzi, Leishmania amazonensis, and Leishmania infatum, as well as the QSAR model for toxicity activity. Most of the evaluated ligands presented high antiparasitic activity. According to the docking results, the family of triazole derivatives presented the best affinity with the different macromolecular targets. The ADME results showed that most of the evaluated compounds present adequate conditions to be administered orally. Naphthoquinone derivatives show good biological activity results, depending on the substituents attached to the quinone ring, and perhaps the potential to be converted into drugs or starting molecules.Fil: Prieto Cárdenas, Lina S.. Universidad Pedagógica y Tecnológica de Colombia; ColombiaFil: Arias Soler, Karen A.. Universidad Pedagógica y Tecnológica de Colombia; ColombiaFil: Nossa González, Diana Lisseth. Universidad Pedagógica y Tecnológica de Colombia; Colombia. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Rozo Núñez, Wilson E.. Universidad Pedagógica y Tecnológica de Colombia; ColombiaFil: Cárdenas-Chaparro, Agobardo. Universidad Pedagógica y Tecnológica de Colombia; ColombiaFil: Duchowicz, Pablo Román. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Instituto de Investigaciones Fisicoquímicas Teóricas y Aplicadas. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Instituto de Investigaciones Fisicoquímicas Teóricas y Aplicadas; ArgentinaFil: Gómez Castaño, Jovanny Arles. Universidad Pedagógica y Tecnológica de Colombia; Colombi

Técnicas analíticas contemporáneas para la identificación de residuos de sulfonamidas, quinolonas y cloranfenicol

The excessive use of drugs in the veterinary industry generates bioaccumulation in animal organs, tissues, muscles and fat. Depending on the concentration, these residues can reach man via the food chain. Food safety comprehends the use of these drugs and their residues such as sulfonamides, chloramphenicol and quinolones, which have been found in different slaughter animals. Some countries have limited regulations to control this issue. The implementation of standards set by the European Union is essential to monitor and control this problem at a national level. In this review, we use analytical techniques to identify the residues produced by these drugs, focusing on recently developed technologies that are essential tools to control this problem. Liquid chromatography combined with mass spectrometry and its various interface systems is the most recommended technology to detect residues in various food matrices

Técnicas analíticas contemporáneas para la identificación de residuos de sulfonamidas, quinolonas y cloranfenicol

The excessive use of drugs in the veterinary industry generates bioaccumulation in animal organs, tissues, muscles and fat. Depending on the concentration, these residues can reach man via the food chain. Food safety comprehends the use of these drugs and their residues such as sulfonamides, chloramphenicol and quinolones, which have been found in different slaughter animals. Some countries have limited regulations to control this issue. The implementation of standards set by the European Union is essential to monitor and control this problem at a national level. In this review, we use analytical techniques to identify the residues produced by these drugs, focusing on recently developed technologies that are essential tools to control this problem. Liquid chromatography combined with mass pectrometry and its various interface systems is the most recommended technology to detect residues in various food matrices

Técnicas analíticas contemporáneas para la identificación de residuos de sulfonamidas, quinolonas y cloranfenicol

The excessive use of drugs in the veterinary industry generates bioaccumulation in animal organs, tissues, muscles and fat. Depending on the concentration, these residues can reach man via the food chain. Food safety comprehends the use of these drugs and their residues such as sulfonamides, chloramphenicol and quinolones, which have been found in different slaughter animals. Some countries have limited regulations to control this issue. The implementation of standards set by the European Union is essential to monitor and control this problem at a national level. In this review, we use analytical techniques to identify the residues produced by these drugs, focusing on recently developed technologies that are essential tools to control this problem. Liquid chromatography combined with mass spectrometry and its various interface systems is the most recommended technology to detect residues in various food matrices

Antiprotozoal QSAR modelling for trypanosomiasis (Chagas disease) based on thiosemicarbazone and thiazole derivatives

Chagas disease, caused by the protozoan parasite Trypanosoma cruzi, remains a neglected endemic infection that affects around 8 million people worldwide and causes 12,000 premature deaths per year. Traditional chemotherapy is limited to the nitro-antiparasitic drugs Benznidazole and Nifurtimox, which present serious side effects and low long-term efficacy. Several research efforts have been made over the last decade to find new chemical structures with better effectiveness and tolerance than standard anti-Chagas drugs. Among these, new sets of thiosemicarbazone and thiazole derivatives have exhibited potent in vitro activity against T. cruzi, especially for its extracellular forms (epimastigote and trypomastigote). In this work, we have developed three antiprotozoal quantitative structure-relationship (QSAR) models for Chagas disease based on the in vitro activity data reported as IC50 (μM) and CC50 (μM) over the last decade, particularly by Lima-Leite's group in Brazil. The models were developed using the replacement method (RM), a technique based on Multivariable Linear Regression (MLR), and external and internal validation methodologies, like the use of a test set, Leave-one-Out (LOO) cross-validation and Y-Randomization. Two of these QSAR models were developed for trypomastigotes form of the parasite Trypanosoma cruzi, one based on IC50 and the other on CC50 data; while the third QSAR model was developed for its epimastigotes form based on CC50 activity. Our models presented sound statistical parameters that endorses their prediction capability. Such capability was tested for a set of 13 hitherto-unknown structurally related aromatic cyclohexanone derivatives.Fil: Nossa González, Diana Lisseth. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Pedagógica y Tecnológica de Colombia; ColombiaFil: Gómez Castaño, Jovanny Arles. Universidad Pedagógica y Tecnológica de Colombia; ColombiaFil: Rozo Núñez, Wilson E.. Universidad Pedagógica y Tecnológica de Colombia; ColombiaFil: Duchowicz, Pablo Román. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Instituto de Investigaciones Fisicoquímicas Teóricas y Aplicadas. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Instituto de Investigaciones Fisicoquímicas Teóricas y Aplicadas; Argentin

INNOVA ITFIP MAGAZINE VOL 5 No. 1

El volumen 5 No. 1 de la revista innova ITFIP da cuenta de los diferentes artículos científicos producto de proyectos de investigación enviados por autores nacionales e internacionales, dando a conocer diversas temáticas que tienen que ver con temas interdisciplinarios relacionados con las ciencias económicas, administrativas, contables, de educación y tecnológicas.Tabla de contenido: ADMINISTRACIÓN MUJERES EMPRESARIAS. EMPODERAMIENTO EMPRESARIAL FEMENINO Y RELACIONES SOCIALES EN AMECA, JALISCO Sara Jazmín Ramírez Guerrero , Myriam Guadalupe Colmenares López 6 LIDERAZGO COMUNITARIO Y SU INFLUENCIA EN LA SOCIEDAD COMO MEJORA DEL ENTORNO RURAL German Enrique Reyes Rojas, Oscar Geovanni Hernández Núñez, Fabio González Díaz 15 EFICIENCIA DE LOS PROCESOS ADMINISTRATIVOS DE LA INGENIERÍA EN INNOVACIÓN Y DESARROLLO EMPRESARIAL DE LA UNIVERSIDAD TECNOLÓGICA DE QUERÉTARO Miriam Liliana Barajas Ruíz, Luis Miguel González García, Yarene Itzel Marín Jimeno 28 EFECTOS DE LA ENTRADA EN EL MERCADO DE TIENDAS ARA EN LOS PEQUEÑOS COMERCIANTES DE LA CIUDAD DE CARTAGENA Armando Batista Castillo , Wilson Darío Guacari Villalba 40 CONTADURÍA IMPACTO SOCIOECONÓMICO DE LOS EGRESADOS DEL PROGRAMA DE CONTADURÍA PÚBLICA DEL CERES DE FLANDES DEL AÑO 2014 AL 2018 Elizabeth Palma Cardoso, Orlando Varón Giraldo, Leidy Johana Aldana, Natalia Camila Yate Rozo 51 AUDITORIA DE USABILIDAD DE HERRAMIENTAS IMPLEMENTADAS EN PLATAFORMAS VIRTUALES PARA OFERTAR SERVICIOS CON RESPONSABILIDAD SOCIAL Olga Inés Ceballos, Luz Amparo Mejía Castellanos, Deicy Arango Medina CIENCIA Y TECNOLOGÍA CONSIDERACIONES PARA APLICAR LOS PRINCIPIOS DE LA TEORÍA DEL ACTOR-RED A LA COMUNICACIÓN PÚBLICA DE LA CIENCIA Y LA TECNOLOGÍA Daniel Martínez Sahagún NORMAS DE PUBLICACIÓN DE LA REVISTA INNOVA ITFIP 64 78 8

Diversidad biológica y cultural del sur de la Amazonia colombiana

La gran cuenca amazónica compartida por Brasil, Colombia, Perú, Bolivia, Venezuela, Ecuador y las tres Guyanas, contiene una de las mayores riquezas biológicas y culturales del planeta y es considerada parte de la seguridad ecológica global. Constituye el 45% de los bosques tropicales del mundo, es una de las áreas silvestres más extensas y de mayor reserva de agua dulce del planeta, su sistema hídrico es el mayor tributario de todos los océanos, alberga aún, cerca de 379 grupos étnicos y en cuanto a endemismo, no existe otra región que se le aproxime. En Colombia, la Amazonia a lo largo de la historia ha sufrido distintos procesos de intervención antrópica: la conquista; la colonización; el auge del caucho y la quina; la explotación maderera, petrolera; la implementación de cultivos de uso ilícito y de sistemas productivos no aptos a las condiciones del medio natural; entre otros, son procesos que han socavado tanto los recursos biológicos como los culturales. Conscientes de la problemática actual de la Amazonia así como de la importancia que reviste para el mundo y para el país, la Corporación para el Desarrollo Sostenible del Sur de la Amazonia –Corpoamazonia– y el Instituto de Investigación de Recursos Biológicos Alexander von Humboldt –IAvH-, firmaron en el año 2004 un convenio con el n de aunar esfuerzos para formular el plan de acción en biodiversidad en la región sur de la Amazonia colombiana (departamentos de Caquetá, Putumayo y Amazonas). El plan de acción, busca posicionar la biodiversidad en el desarrollo regional y contribuir a un mayor conocimiento y a unas mejores prácticas de conservación y utilización sostenible de los recursos biológicos y culturales de este importante espacio geográfico. Desarrolla a escala regional, la Política Nacional en Biodiversidad y la Propuesta Técnica de Plan de Acción Nacional en Biodiversidad – Biodiversidad siglo XXI -